Abstract
Six novel potential PARP1 inhibitors were identified by means of substructure search and molecular docking into PAPR1 active site; one compound (STK970217) potentiated the cytotoxicity of doxorubicin in hepatocellular carcinoma HepG2 cells being non-cytotoxic as a single agent, while three other identified compounds inhibited the growth of HepG2 cells both individually and in combination with doxorubicin.
References
1.
D’AMOURS D., DESNOYERS S., D’SILVA I., POIRIER G.G.
Biochemical Journal,
1999
2.
Olaussen K.A., Adam J., Vanhecke E., Vielh P., Pirker R., Friboulet L., Popper H., Robin A., Commo F., Thomale J., Kayitalire L., Filipits M., Le Chevalier T., André F., Brambilla E., et. al.
Lung Cancer,
2013
3.
Treatment with the PARP-inhibitor PJ34 causes enhanced doxorubicin-mediated cell death in HeLa cells
Magan N., Isaacs R.J., Stowell K.M.
Anti-Cancer Drugs,
2012
4.
5.
Novikov F.N., Stroylov V.S., Stroganov O.V., Kulkov V., Chilov G.G.
Journal of Molecular Modeling,
2009
6.
Romashov L.V., Zeifman A.A., Zakharenko A.L., Novikov F.N., Stroilov V.S., Stroganov O.V., Chilov G.G., Khodyreva S.N., Lavrik O.I., Titov I.Y., Svitan’ko I.V.
Mendeleev Communications,
2012
7.
Stroganov O.V., Novikov F.N., Stroylov V.S., Kulkov V., Chilov G.G.
Journal of Chemical Information and Modeling,
2008
8.
10.1016/j.mencom.2015.09.016_bib0040
Mosmann
Methods,
1983
9.
BLISS C.I.
Annals of Applied Biology,
1939
10.
10.1016/j.mencom.2015.09.016_bib0050
Huang
Oncol. Rep.,
2008
11.
Muñoz-Gámez J.A., Quiles-Pérez R., Ruiz-Extremera A., Martín-Álvarez A.B., Sanjuan-Nuñez L., Carazo A., León J., Oliver F.J., Salmerón J.
Cancer Letters,
2011